Manufacturer:

Sunovion

Pharmacological Class:

Atypical antipsychotic (benzoisothiazol derivative).

Active Ingredient(s):

Lurasidone 40mg, 80mg; tabs.

Indication(s):

Schizophrenia.

Pharmacology:

The mechanism of action of lurasidone, as with other drugs having efficacy in schizophrenia, is unknown. It has been suggested that the efficacy of lurasidone in schizophrenia is mediated through a combination of central dopamine Type 2 (D₂) and serotonin Type 2 (5HT_2A) receptor antagonism.

Clinical Trials:

The efficacy of lurasidone was established in 4 short-term (6-week), placebo-controlled studies in adults who met DSM-IV criteria for schizophrenia. One study included an active-control arm (olanzapine) to assess assay sensitivity. The Positive and Negative Syndrome Scale (PANSS), Brief Psychiatric Rating Scale derived (BPRSd), and Clinical Global Impression severity scale (CGI-S) were used for assessing psychiatric signs and symptoms. The endpoint associated with each instrument was change from baseline in the total score to the end of Week 6.

In a 6-week, placebo-controlled trial involving two fixed doses of lurasidone (40 or 120mg/day), both doses of lurasidone at endpoint were superior to placebo on the BPRSd total score, and the CGI-S, as was lurasidone 80mg/day in another 6-week placebo-controlled trial.

In a 6-week, placebo and active-controlled trial involving two fixed doses of lurasidone (40 or 120mg/day) and an active control (olanzapine), both lurasidone doses and the active control at endpoint were superior to placebo on the PANSS total score, and the CGI-S.

In a 6-week, placebo-controlled trial involving three fixed doses of lurasidone (40, 80 or 120mg/day), only the 80mg/day dose of lurasidone at endpoint was superior to placebo on the PANSS total score, and the CGI-S.

Thus, the efficacy of lurasidone at doses of 40, 80 and 120mg/day was established in two studies for each dose. However, the 120mg dose did not appear to add additional benefit over the 40mg dose.

Legal Classification:

Rx

Adults:

Take with food (≥350 calories). 40mg once daily. Max 80mg/day. Moderate to severe renal or hepatic impairment, concomitant moderate CYP3A4 inhibitors: max 40mg/day.

Children:

Not recommended.

Contraindication(s):

Concomitant strong CYP3A4 inhibitors (eg, ketoconazole) and inducers (eg, rifampin).

Warnings/Precautions:

Elderly (not for dementia-related psychosis); increased risk of death. Discontinue if neuroleptic malignant syndrome (NMS) occurs; consider discontinuing if tardive dyskinesia occurs. Cardio- or cerebrovascular disease. Pre-existing low WBCs or history of leukopenia/neutropenia; monitor CBCs during 1^st few months of therapy; discontinue if WBCs decline. Moderate to severe hepatic or renal impairment. Diabetes risk factors (obtain baseline fasting blood sugar). Monitor for hyperglycemia, dyslipidemia, weight gain, hyperprolactinemia. History of seizures. Exposure to extreme heat. Dysphagia. Write Rx for smallest practical amount. Pregnancy (Cat.B). Nursing mothers.

Interaction(s):

See Adults and Contraindications. Additive CNS effects with alcohol, other CNS depressants.

Adverse Reaction(s):

Somnolence, akathisia, nausea, parkinsonism, agitation; orthostatic hypotension, syncope, hyperglycemia, dyslipidemia, weight gain, hyperprolactinemia, leukopenia/neutropenia, possible NMS, tardive dyskinesia.

How Supplied:

Tabs—28 (4 blister cards x 7 tabs), 30, 90, 500

Last Updated:

6/22/2011